Asymmetric triplex metallohelices with high and selective activity against cancer cells

Small cationic amphiphilic α-helical peptides are emerging as agents for the treatment of cancer and infection, but they are costly and display unfavourable pharmacokinetics. Helical coordination complexes may offer a three-dimensional scaffold for the synthesis of mimetic architectures. However, the high symmetry and modest functionality of current systems offer little scope to tailor the structure to interact with specific biomolecular targets, or to create libraries for phenotypic screens. Here, we report the highly stereoselective asymmetric self-assembly of very stable, functionalized metallohelices. Their anti-parallel head-to-head-to-tail ‘triplex’ strand arrangement creates an amphipathic functional topology akin to that of the active sub-units of, for example, host-defence peptides and ​p53. The metallohelices display high, structure-dependent toxicity to the human colon carcinoma cell-line HCT116 ​p53++, causing dramatic changes in the cell cycle without DNA damage. They have lower toxicity to human breast adenocarcinoma cells (MDA-MB-468) and, most remarkably, they show no significant toxicity to the bacteria methicillin-resistant Staphylococcus aureus and Escherichia coli. At a glanc

The mechanisms of boronate ester formation and fluorescent turn-on in ortho-aminomethylphenylboronic acids

ortho-Aminomethylphenylboronic acids are used in receptors for carbohydrates and various other compounds containing vicinal diols. The presence of the o-aminomethyl group enhances the affinity towards diols at neutral pH, and the manner in which this group plays this role has been a topic of debate. Further, the aminomethyl group is believed to be involved in the turn-on of the emission properties of appended fluorophores upon diol binding. In this treatise, a uniform picture emerges for the role of this group: it primarily acts as an electron-withdrawing group that lowers the pK(a) of the neighbouring boronic acid thereby facilitating diol binding at neutral pH. The amine appears to play no role in the modulation of the fluorescence of appended fluorophores in the protic-solvent-inserted form of the boronic acid/boronate ester. Instead, fluorescence turn-on can be consistently tied to vibrational-coupled excited-state relaxation (a loose-bolt effect). Overall, this Review unifies and discusses the existing data as of 2019 whilst also highlighting why o-aminomethyl groups are so widely used, and the role they play in carbohydrate sensing using phenylboronic acids

23-tól 30-ig Prolongálva! - Előadások kezdete 5 órától folytatólag

Szöveges plakát, melyet széles sávokban szecesziós keret határol. A mozi "Carmen" felirata egy szalagon olvasható. Fölötte filmtekercs kanyarog. A keretet sűrű növényi ornamentika, virágok és levelek alkotják. Színek: mustársárga, sötétkék és fekete, fehér

SDSS J211852.96−073227.5: The first non-local, interacting, late-type intermediate Seyfert galaxy with relativistic jets

It has been often suggested that a tangible relation exists between relativistic jets in active galactic nuclei (AGN) and the morphology of their host galaxies. In particular, relativistic jets may commonly be related to merging events. Here we present for the first time a detailed spectroscopic and morphological analysis of a Seyfert galaxy, SDSS J211852.96−073227.5, at z = 0.26. This source has previously been classified as a gamma-ray emitting narrow-line Seyfert 1 galaxy. We re-observed it with the 6.5 m Clay Telescope and these new, high-quality spectroscopic data have revealed that it is actually an intermediate-type Seyfert galaxy. Furthermore, the results of modelling the Ks-band near-infrared images obtained with the 6.5 m Baade Telescope indicate that the AGN is hosted by a late-type galaxy in an interacting system, strengthening the suggested connection between galaxy interactions and relativistic jets